Abstract: Compounds of the formula
are useful for the treatment of anxiety, depression and related CNS disorders and other conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.
Type:
Grant
Filed:
December 13, 1999
Date of Patent:
June 5, 2001
Assignee:
American Home Products Corporation
Inventors:
Michael Gerard Kelly, Lynne Padilla Greenblatt, Frances Christy Nelson
Abstract: Compounds of the formula
are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders and neurodegenerative diseases.
Abstract: This invention provides, low molecular weight, non-peptide inhibitors of matrix metalloproteinases and TNF-&agr; converting enzyme (TACE, tumor necrosis factor-&agr; converting enzyme) of formula:
B
wherein B is
P and Q are
provided that when
P is
Q is
and vice versa;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 14, 1998
Date of Patent:
May 8, 2001
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
Abstract: Compounds of the formula:
are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
May 1, 2001
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
Abstract: Novel, stable formulations of bupropion hydrochloride are provided which will maintain at least 80% of initial bupropion hydrochloride potency after one year. Methods of inhibiting degradation of bupropion hydrochloride and methods of preparing stable formulations of bupropion hydrochloride are also provided.
Type:
Grant
Filed:
December 30, 1997
Date of Patent:
April 24, 2001
Assignee:
American Home Products Corporation
Inventors:
Amitava Maitra, Prakash Shriram Kulkarni, Bharat Bhogilal Shah, Joseph Michael DeVito
Abstract: Compounds of the formula
R1 and R2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R3 is hydrogen, alkyl of 1 to 6 carbon atoms, or cycloalkyl of 3 to 10 carbon atoms; and R4 is phenyl or naphthyl substituted with alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or NR5R6; substituted or unsubstituted phenylalkyl wherein the alkyl group contains 1 to 6 carbon atoms; substituted or unsubstituted 5 to 10 membered heteroaryl having 1 to 3 heteroatoms selected from N, S and O; substituted or unsubstituted cycloalkyl of 3 to 10 carbon atoms; or substituted or unsubstituted cycloalkylalkyl of 4 to 10 carbon atoms; provided that phenyl or naphthyl is substituted with NR5R6 when R1 and R2 is alkyl, are useful in the treatment of various disorders associated bone loss by increased transcription and elevation of plasma calcitonin levels.
Type:
Grant
Filed:
May 3, 1999
Date of Patent:
April 24, 2001
Assignee:
American Home Products Corporation
Inventors:
Adam Matthew Gilbert, Gerardo Francisco, Magda Asselin
Abstract: Compounds of the formula:
are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.
Type:
Grant
Filed:
November 22, 1999
Date of Patent:
March 27, 2001
Assignee:
American Home Products Corporation
Inventors:
Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
Abstract: The invention is a method of treatment for the relief of an addictive, compulsive disorder which comprises the administration to a human or animal suffering from such a disorder an effective amount of the compound of the formula:
wherein R is hydrogen, alkyl (C1-C6); R1 is hydrogen, mono or disubstituted halogen, alkoxy (C1-C3), CF3, alkyl (C1-C6); and R2 is hydrogen, methyl or ethyl, or a pharmaceutically acceptable salt thereof.
Abstract: Compounds of the formula:
are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simples viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses −6 and −7, and Kaposi herpes virus.
Type:
Grant
Filed:
November 22, 1999
Date of Patent:
March 13, 2001
Assignee:
American Home Products Corporation
Inventors:
Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
Abstract: Compounds of the formula:
are useful in treating disease conditions mediated by TNF-&agr; such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
March 13, 2001
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, James M. Chen, Frances C. Nelson
Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.
Type:
Grant
Filed:
August 26, 1998
Date of Patent:
March 6, 2001
Assignee:
American Cyanamid Company
Inventors:
Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Jannie Lea Baker, Jeremy Ian Levin
Abstract: Sterile pharmaceutical compositions parenteral administration containing propofol in an oil-in-water emulsion additionally containing an amount of the preservative tromethamine sufficient to prevent signficant growth of microorganisms for at least 24 hours after extrinsic contamination.
Type:
Grant
Filed:
March 24, 1999
Date of Patent:
January 23, 2001
Assignee:
American Home Products Corporation
Inventors:
Mary Mathew George, Pui-Ho Yuen, Martin A. Joyce
Abstract: Compounds having the formula
R5O—A—NR4—R2 (V)
where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).
Type:
Grant
Filed:
January 22, 1998
Date of Patent:
January 16, 2001
Assignee:
John Wyeth & Brother Ltd.
Inventors:
Christopher Ian Brightwell, Robin Gerald Shepherd
Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
Type:
Grant
Filed:
February 19, 1998
Date of Patent:
January 9, 2001
Assignee:
American Cyanamid Company
Inventors:
Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula
wherein:
R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl;
R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2;
n is 0 or 1;
R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons;
and all crystalline forms and the pharmaceutically acceptable salts thereof.
Abstract: Compounds of the formula ##STR1## are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
Type:
Grant
Filed:
November 22, 1999
Date of Patent:
December 26, 2000
Assignee:
American Home Products Corporation
Inventors:
Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.
Type:
Grant
Filed:
June 11, 1999
Date of Patent:
December 19, 2000
Assignee:
American Cyanamid Company
Inventors:
Jeremy Ian Levin, Frances Christy Nelson
Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.